Screening of σ2 Receptor Ligands and In Vivo Evaluation of 11C-Labeled 6,7-Dimethoxy-2-[4-(4-methoxyphenyl)butan-2-yl]-1,2,3,4-tetrahydroisoquinoline for Potential Use as a σ2 Receptor Brain PET Tracer

Kim, Ho Young; Lee, Ji Youn; Hsieh, Chia-Ju; Riad, Aladdin; Izzo, Nicholas J.; Catalano, Susan M.; Graham, Thomas J. A.; Mach, Robert H.

doi:10.1021/acs.jmedchem.2c00191

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Screening of σ2 Receptor Ligands and In Vivo Evaluation of 11C-Labeled 6,7-Dimethoxy-2-[4-(4-methoxyphenyl)butan-2-yl]-1,2,3,4-tetrahydroisoquinoline for Potential Use as a σ2 Receptor Brain PET Tracer

Kim, Ho Young, Lee, Ji Youn, Hsieh, Chia-Ju, Riad, Aladdin, Izzo, Nicholas J., Catalano, Susan M., Graham, Thomas J. A., Mach, Robert H.·2022·Journal of Medicinal Chemistry

DOI 10.1021/acs.jmedchem.2c00191PMC PMC13012568

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In the retina, S2R is expressed in retinal pigment epithelium cells, photoreceptors, and retinal ganglion cells.
“In the retina, S2R is expressed in several cell types including the retinal pigment epithelium cells, photoreceptors, and retinal ganglion cells [70,71,72,73,74].”
From Sigma-2 Receptors—From Basic Biology to Therapeutic Target: A Focus on Age-Related Degenerative Diseases (2023) · cites this paper as [74]

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Structures of the σ2 receptor enable docking for bioactive ligand discovery
Alon, A., Lyu, J., Braz, J. M., Tummino, T. A., Craik, V., O’Meara, M. J., Webb, C. M., Radchenko, D. S., Moroz, Y. S., Huang, X.-P., et al. (2021) · Nature · doi:10.1038/s41586-021-04175-x · Cited by 211
Alzheimer's Therapeutics Targeting Amyloid Beta 1–42 Oligomers I: Abeta 42 Oligomer Binding to Specific Neuronal Receptors Is Displaced by Drug Candidates That Improve Cognitive Deficits
Izzo, N. J., Staniszewski, A., To, L., Fa, M., Teich, A. F., Saeed, F., Wostein, H., Walko, T., Vaswani, A., Wardius, M., et al. (2014) · PLoS ONE · doi:10.1371/journal.pone.0111898 · Cited by 180
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Sigma-2 Receptor/TMEM97 and PGRMC-1 Increase the Rate of Internalization of LDL by LDL Receptor through the Formation of a Ternary Complex
Riad, A., Zeng, C., Weng, C.-C., Winters, H., Xu, K., Makvandi, M., Metz, T., Carlin, S., & Mach, R. H. (2018) · Scientific Reports · doi:10.1038/s41598-018-35430-3 · Cited by 147
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The Sigma-2 Receptor/TMEM97, PGRMC1, and LDL Receptor Complex Are Responsible for the Cellular Uptake of Aβ42 and Its Protein Aggregates
Riad, A., Lengyel-Zhand, Z., Zeng, C., Weng, C.-C., Lee, V. M.-Y., Trojanowski, J. Q., & Mach, R. H. (2020) · Molecular Neurobiology · doi:10.1007/s12035-020-01988-1 · Cited by 81
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Sigma-2 Receptors—From Basic Biology to Therapeutic Target: A Focus on Age-Related Degenerative Diseases
Lizama, B. N., Kahle, J., Catalano, S. M., Caggiano, A. O., Grundman, M., & Hamby, M. E. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24076251 · Cited by 54
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Authors: Kim, H. Y., Lee, J. Y., Hsieh, C.-J., Riad, A., Izzo, N. J., Catalano, S. M., Graham, T. J. A., & Mach, R. H.
Affiliations: Department of Radiology, University of Pennsylvania, Vagelos Laboratories, 1012, 231 South 34th Street, Philadelphia, Pennsylvania 19104-6323, United States
Cognition Therapeutics Inc., Pittsburgh, Pennsylvania 15203-5118, United States
ORCID: Kim, Ho Young
Hsieh, Chia-Ju
Riad, Aladdin
Izzo, Nicholas J.
Mach, Robert H.
Venue: Journal of Medicinal Chemistry
Publisher: American Chemical Society (ACS)
Published: 2022-04-11
Volume: 65
Issue: 8
Pages: 6261-6272
ISSN: 0022-2623
1520-4804
DOI: 10.1021/acs.jmedchem.2c00191
PMC: PMC13012568
Cited by: 16
References: 4
Language: en
Licence: doi.org/10.15223/policy-029 (stm-asf)
doi.org/10.15223/policy-037 (stm-asf)
doi.org/10.15223/policy-045 (stm-asf)
Funders: National Institutes of Health (R42AG052249)

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Screening of σ2 Receptor Ligands and In Vivo Evaluation of 11C-Labeled 6,7-Dimethoxy-2-[4-(4-methoxyphenyl)butan-2-yl]-1,2,3,4-tetrahydroisoquinoline for Potential Use as a σ2 Receptor Brain PET Tracer

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